• Title/Summary/Keyword: Antibacterial compound

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Synthesis and Biological Evaluation of 2-Amino-4H-pyran-3,4,5-tricarboxylate Salt Derivatives

  • Akbari, Ali;Azami-Sardooei, Zabihollah;Hosseini-Nia, Asghar
    • Journal of the Korean Chemical Society
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    • v.57 no.4
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    • pp.455-460
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    • 2013
  • A novel and simple method for the synthesis of 2-amino-4H-pyran-3,4,5-tricarboxylate derivative and the evaluation of their antibacterial activity against Pseudomonas syringae, Xanthomonas citi and Pectobacterium carotovorum are reported. The structure of the isolated compounds has been determined by means of $^1H/^{13}C$ NMR and FT-IR Spectroscopy. The reaction of alkyl isocyanides with acetylenic esters in the presence of dimethyl acetone-1,3-dicarboxylate in the present of $BF_3.SiO_2$ at ambient temperature. Some of the compound showed significant inhibition to growth of bacteria.

Organizational Capabilities for Effective Knowledge Creation: An In-depth Case Analysis of Quinolone Antibacterial Drug Discovery Process (효과적 지식창출을 위한 조직능력 요건: 퀴놀론계 항생제 개발 사례를 중심으로)

  • Lee, Chun-Keun;Kim, Linsu
    • Knowledge Management Research
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    • v.2 no.1
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    • pp.109-132
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    • 2001
  • The purpose of this article is to develop a dynamic model of organizational capabilities and knowledge creation, and at the same time identify the organizational capability factors for effective knowledge creation, by empirically analyzing the history of new Quinolone antibacterial drug compound (LB20304a) discovery process at LG, as a case in point. Major findings of this study are as follows. First, in a science-based area such as drug development, the core of successful knowledge creation lies in creative combination of different bodies of scientific explicit knowledge. Second, the greater the difficulty of learning external knowledge, the more tacit knowledge is needed for the recipient firm to effectively exploit that knowledge. Third, in science-based sector such as pharmaceutical industry, the key for successful knowledge creation lies in the capability of recruiting and retaining star scientists. Finally, for effective knowledge creation, a firm must keep its balance among three dimensions of organizational capabilities: local, process, architectural capabilities.

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Studies on Some Bioactive 1,1-Bis(2-benzylidene-5-aryliden-1,3-thiadiazolidin-4-one)cyclopropane

  • Panwar, Hemant;Chaudhary, Nidhi;Singh, Sachi;Chawla, Amit
    • Journal of the Korean Chemical Society
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    • v.55 no.6
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    • pp.994-999
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    • 2011
  • Some novel heterocyclic derivatives of 1,1-bis(2-phenyl-5-arylidine-1,3-thiadiazolidin-4-one)cyclopropane 4(a-i) have been synthesized from cyclopropane dicarboxylic acid and substituted thiadiazole moieties. All the synthesized compounds have been characterized by elemental and spectral (I.R., $^1H$-NMR, Mass) analysis. Furthermore, above said compounds were screened for their antifungal and antibacterial activities. Compound 4c was found the most potent one which further evaluated for lesser toxicity test.

Synthesis, Characterization and Antimicrobial Activity of Bifunctional Sulfonamide-Amide Derivatives

  • Abbavaram, Babul Reddy A.;Reddyvari, Hymavathi R.V.
    • Journal of the Korean Chemical Society
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    • v.57 no.6
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    • pp.731-737
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    • 2013
  • A convenient synthesis of bifunctional sulfonamide-amide derivatives was reported. Amide coupling of 4-methyl benzoic acid 1 followed by reaction with chlorosulfonic acid produce ethyl-4-(3-(chlorosulfonyl)-4-methylbenzoyl)piperazine-1-carboxylate 4. The resulted compound on further treatment with various anilines produces the title sulfonamide-amide derivatives 5a-n. The configurations of these compounds were established by elemental analysis, IR, $^1H$ NMR, mass spectra, and by their preparation from the corresponding 4-methyl benzoic acid 1 and chlorosulfonic acid. All these new compounds demonstrate significant in vitro antibacterial and antifungal activities against all bacterial and fungal strains.

Studies on the Constituents of Berberis amurensis Ruprecht (매발톱나무의 성분에 관한 연구)

  • Lee, Hyang-Yi;Kim, Chong-Won
    • Korean Journal of Pharmacognosy
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    • v.28 no.4
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    • pp.257-263
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    • 1997
  • Berberis amurensis Ruprecht(Berberidaceae) is a medicinal plant indigenous to the middle and northern part of Korean peninsula. The woody parts of this plant have been used for the ocular, peptic and intestinal disorders. The stems of this plants were extracted with MeOH and the MeOH extract was partitioned between organic phases and water layer, successively to fractionated quarternary alkaloids. The acetone-soluble part of guarternary alkaloidal fraction had antibacterial activities and it contained four protoberberine alkaloids such as palmatine(I), Berberine(II), Jatrorrhizine(III) and coptisine(IV), and one aporphine alkaloid, magnoflorine(V). Although the isolations of the compounds I, II, IIII, IV and V from different sources were reported, this is the first report that Berberis amurensis contained the compounds. When the contents of compound I(palmatine) and II(berberine) were quantified and compared with those of other plant parts, cortex contained higher palmatine and berberine than any other part of the plant.

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Clinical evaluation of cetylpyridinium chloride-containing mouthwash in halitosis

  • Kang, Minkyung;Kim, Boyeon;Park, Hyounggeun;Lee, Eunseok
    • International Journal of Oral Biology
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    • v.44 no.1
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    • pp.27-29
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    • 2019
  • Halitosis is a very common disease that affects the majority of the population and is characterized by unpleasant odor during expiration. Anaerobic bacteria produce a range of malodorous substances including volatile sulfur compounds. To reduce oral malodor, the amount of oral microorganisms should be managed through brushing, scraping, and use of antibacterial agents. In this study, a mouthwash containing 0.05% cetylpyridinium chloride was tested on 22 candidates with oral malodor for two weeks to confirm oral malodor reduction through the use of antibacterial mouthwashes. Volatile sulfur compound measurements were significantly lower after using the mouthwash than before using it; thus, the mouthwash effectively reduced oral malodor.

Antimicrobial Terpenoids from Seed of Chamaecyparis obtusa (Siebold & Zucc.) Endl.

  • Bo Shi Liu;Jung Eun Kim;Nam Ho Lee
    • Journal of the Korean Chemical Society
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    • v.68 no.4
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    • pp.199-204
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    • 2024
  • Chamaecyparis obtusa (Siebold & Zucc.) Endl. is an evergreen tree of the family Cupressaceae well known for its unique scents. The seed extract of this cypress tree was phytochemically investigated to isolate a novel abietane-diterpene compound (1) along with fifteen known terpenoids (2-16). All of the isolated compounds were subjected to the screening of antimicrobial activities against Cutibacterium acnes and Staphylococcus epidermidis including erythromycin resistant strains. Among the isolates, 1α-hydroxy-hinokione (1), hinokione (3), 1,2-dehydrohinokione (4) and ferruginol (9) showed significant antibacterial activities against both acne-causing strains. This study demonstrated that abietane-type diterpenoids are the main antibacterial components in C. obtusa seed extract, and some isolated compounds can be further developed as potential acne-treatment agents.

A Novel Bromoindole Alkaloid from a Korean Colonial Tunicate Didemnum sp.

  • Hahn, Dongyup;Kim, Geum Jin;Choi, Hyukjae;Kang, Heonjoong
    • Natural Product Sciences
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    • v.21 no.4
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    • pp.278-281
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    • 2015
  • Chemical investigation on a colonial marine tunicate, Didemnum sp. led to the isolation of a series of indole alkaloids including a new (1) and two known metabolites (2-3). Based on the spectroscopic analysis including 1D and 2D NMR along with MS spectra, the structure of 1 (16-epi-18-acetyl herdmanine D) was elucidated as a new amino acid derivative. The absolute configuration of 1 was determined by comparison of specific rotation with the known compound. The structures of compounds 2 and 3 were also identified as bromoindole containing compounds N-(6-bromo-1H-indole-3-carbonyl)-L-arginine and (6-bromo-^1H-indol-3-yl) oxoacetamide, respectively, based on $^1H$ and $^{13}C$ NMR data, MS data and specific rotation value. Their pharmacological potentials as antibacterial agents and FXR antagonists were investigated, but no significant activity was found. However, the structural similarity of compound 1 to compound 4 suggested the anti-inflammatory potential of compound 1.

Antibacterial Substances of the Flower of Chrysanthemum zawadskii Herbich var. latilobum Kitamura (구절초 꽃의 항균성 물질)

  • Jang, Dae-Sik;Park, Ki-Hun;Choi, Sang-Uk;Nam, Sang-Hae;Yang, Min-Suk
    • Applied Biological Chemistry
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    • v.40 no.1
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    • pp.85-88
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    • 1997
  • In orther to isolate antibacterial substances from the flower of Chrysanthemum zawadskii Herbich var. latilobum Kitam., the chloroform fraction was fractionated according to the activity against B. subtilis, S. aureus and V. parahaemolyticus. Two antibacterial substances were isolated and purified by preparative TLC and recrystallization. Compound I showed activity against all the tested bacteria and compound II exhibited the activity against B. subtilis and v. parahaemolyticus except S. aureus. Compared to benzoic acid and sorbic acid which are being used as food preservatives, compounds I and II showed about five-fold stronger antibacterial activity against B. subtilis and V. parahaemolyticus. On the basis of spectrometric studies including $^1H-NMR,\;^{13}C-NMR,\;DEPT,\;^1H-^1H\;COSY,\;^{13}C-^1H\;COSY$ and Mass, compounds I and II were identified as angeloylcumambrin B and cumambrin A, respectively. This is the first report of the isolation of angeloylcumambrin B and cumambrin A from this plant.

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Synergistic Effects of the Combination of 20-Hydroxyecdysone with Ampicillin and Gentamicin Against Methicillin-Resistant Staphylococcus aureus

  • Kim, Eun-Sook;Jeong, Seung-Il;Kim, Jung-Hoon;Park, Channy;Kim, Shin-Moo;Kim, Jin-Kyung;Lee, Kang-Min;Lee, Sang-Heon;So, Hong-Seob;Park, Ra-Kil
    • Journal of Microbiology and Biotechnology
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    • v.19 no.12
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    • pp.1576-1581
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    • 2009
  • The emergence of methicillin-resistant Staphylococcus aureus (MRSA) has led to an urgent need for the discovery and development of new antibacterial agents. As part of an ongoing investigation into the antibacterial properties of natural products, 20-hydroxyecdysone (20E), isolated from the roots of Achyranthes japonica Nakai, was found to be active against MRSA, either alone or in combination with ampicillin (AM) or gentamicin (GM), via checkerboard assay. This study investigated the antibacterial activity of 20E, which exhibited poor antibacterial activity ($MIC=250-500\;{\mu}g/ml$) against MRSA tested. The combined activity of AM or GE plus 20E against MRSA resulted in fractional inhibitory concentractions (FICs) ranging from 4.00 to $0.031\;{\mu}g/ml$, respectively. Meanwhile, the FIC index ranged from 0.16-4.50, indicating a marked synergistic relationship between AM, GE, and 20E against MRSA. Time-kill assays also showed a remarkable decrease between the combination and the more active compound. Therefore, this study demonstrated that AM, GE, and 20E can act synergistically in inhibiting MRSA in vitro.